Preliminary Study On Sustained Release Tablets Of Acorus Gramineus Antiepileptic Effective Components Combined Borneol

Objective:to study the forming technology of Sustained Release Tablets which optimization prescription was selected by Pharmacodynamics of Borneol combined benzine extracted from acorus gramineus and embeded byβ-CD; and study its quality criteria and stability.Method:(1)Latency to convulsions, seizures, mortality tracking indicators for the efficacy, active ingredients and effective components to Acorus gramineus antiepilepsy and the ratio of borneol to determine the best recipe of antiepilepsy effect;(2)Select the best technology by Orthgonal design amount of water, extraction time, herbs crushing impact of volatile oil degree of extraction factors; (3)Application of uniform design volatile oilβ-CD inclusion and inclusion for high temperature, high humidity, bright light and other factors affecting the stability; (4) The preparation formula was confirmed through optimizing the match of the adjuvant which selected by hydrophilia gel-matrix technique and orthogonal experiment with index of delivery degree,and the mathematic model for the cumulated release-time profile of the tablete was fitted; (5) Toβ-asarone content which was determined by HPLC as an indicator of the quality control of sustained-release tablets;(6)Accelerated test method (temperature:40℃, Humidity:75%, dark conditions) investigated the initial stability of the sustained-release tablets.Results:(1)volatile oil combained with Borneol group could significantly prolong the latent period of convulsion, reduce the rate of acute PTZ seizures and mortality rate in rats;(2)volatile oil extraction process best:most coarse herbs Acorus gramineus, plus 8 times the amount of water, soaking 0.5h, reflux extraction 8h, volatile oil extraction rate of 2.5%;(3)optimum embeded process:volatile oil:β-CD for the (1:3); oil: water (1:15); inclusion temperature:30℃; mixing time:3. 0h; from the inclusion oil content reached 26.99%, volatile oil inclusion rate of 89.58%; (4) best forming process consists of:40% of inclusion volatile oil, borneol 13%, HPMC 30%, EC16%,1% magnesium stearate; (5) sustained-release tablets are formulated for each film ofβ-asarone content of 32mg,the limit concentration of the labeled amount of 90% to 110%; in 2h,6h,12h of the cumulative release rate (Q) were labeled amount should be 15% to 25%,45% to 65% and 85%; (6) volatile oil components in three different months was stable, but borneol sublimation is serious.Conclusion:The technology of this sustained tablet preparation is steady and feasible, the quality is stable and controllable, and can be released slowly in vitro.